EFFECT OF HUMAN SERUM ON THE IN-VITRO ANTI-HIV-1 ACTIVITY OF 1-[(2-HYDROXYETHOXY)METHYL]-6-(PHENYLTHIO)THYMINE (HEPT) DERIVATIVES AS RELATED TO THEIR LIPOPHILICITY AND SERUM-PROTEIN BINDING

Authors
BABA M YUASA S NIWA T YAMAMOTO M YABUUCHI S TAKASHIMA H UBASAWA M TANAKA H MIYASAKA T WALKER RT BALZARINI J DECLERCQ E SHIGETA S
Citation
M. Baba et al., EFFECT OF HUMAN SERUM ON THE IN-VITRO ANTI-HIV-1 ACTIVITY OF 1-[(2-HYDROXYETHOXY)METHYL]-6-(PHENYLTHIO)THYMINE (HEPT) DERIVATIVES AS RELATED TO THEIR LIPOPHILICITY AND SERUM-PROTEIN BINDING, Biochemical pharmacology, 45(12), 1993, pp. 2507-2512
Citations number
29
Categorie Soggetti
Pharmacology & Pharmacy",Biology
Journal title
Biochemical pharmacology → ACNP
ISSN journal
00062952
Volume
45
Issue
12
Year of publication
1993
Pages
2507 - 2512
Database
ISI
SICI code
0006-2952(1993)45:12<2507:EOHSOT>2.0.ZU;2-Y
Abstract
Several derivatives of 10[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymi ne (HEPT) were examined for their inhibitory effects on the replicatio n of human immunodeficiency virus type 1 (HIV-1) in MT-4 cells in the presence of various concentrations (10-50%) of human serum (HS). Altho ugh all HEPT derivatives proved to be highly potent inhibitors of HIV- 1 in the presence of 10% fetal bovine serum, some of them were less in hibitory to HIV-1 replication in the presence of HS. The HEPT derivati ves were found to be highly bound to HS proteins. Both the anti-HIV-1 activity and HS protein binding of the compounds appeared to be relate d to their lipophilicity.